设计和评价琥珀酰化大豆蛋白片剂作为缓控释给药系统。
Design and evaluation of succinylated soy protein tablets as delayed drug delivery systems.
机构信息
Chaire de Recherche du Canada sur les Protéines, les Biosystèmes et les Aliments Fonctionnels, Institut des Nutraceutiques et Aliments Fonctionnels (INAF), Faculté des Sciences de l'Agriculture et de l'Alimentation, Université Laval, Pavillon Paul Comtois, Québec G1K7P4, Canada.
出版信息
Int J Biol Macromol. 2009 Nov 1;45(4):414-20. doi: 10.1016/j.ijbiomac.2009.06.013. Epub 2009 Jul 2.
The impact of succinylation on soy proteins as excipients for delayed delivery of drugs in the gastrointestinal tract was studied. Succinylation decreased protein solubility and protein charge density at pH 1.2 and increased solubility and zeta potential at pH above 4.5. Tablet erosion and swelling were decreased at pH 1.2 and increased at pH 7.5. FTIR analysis indicated polypeptide chain unfolding as a result of succinylation. Tablets of protein succinylated 50% or 100% released less than 10% of loaded riboflavin or rifampicin in 2h at gastric pH in the presence of pepsin but released these compounds rapidly at intestinal pH. Succinylated soy protein tablets were thus gastroresistant, suggesting their use as excipients for controlled release of medicinal or nutraceutical agents.
研究了琥珀酰化对大豆蛋白作为药物在胃肠道内延迟释放的辅料的影响。琥珀酰化降低了蛋白质在 pH 值为 1.2 时的溶解度和蛋白质电荷密度，而在 pH 值高于 4.5 时则增加了溶解度和 ζ 电位。在 pH 值为 1.2 时，片剂的侵蚀和膨胀减少，而在 pH 值为 7.5 时则增加。傅里叶变换红外光谱分析表明，琥珀酰化导致多肽链展开。在胃 pH 值存在胃蛋白酶的情况下，琥珀酰化 50%或 100%的大豆蛋白片剂在 2 小时内释放的负载核黄素或利福平少于 10%，但在肠道 pH 值下迅速释放这些化合物。因此，琥珀酰化大豆蛋白片剂具有胃耐受力，表明它们可用作药物或营养药物控释的辅料。
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